2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Rivanicline hydrochloride

Rivanicline hydrochloride  (Synonyms: RJR-2403 hydrochloride; Metanicotine hydrochloride)

目录号: HY-13225H
产品使用指南 技术支持

Rivanicline (RJR-2403) hydrochloride 是一种神经元型烟碱受体(neuronal nicotinic receptor) 激动剂。Rivanicline hydrochloride 对大鼠大脑皮层的 nAChR (Ki = 26 nM，EC50 为 732 nM) 和 α4β2 亚型(Ki = 26 nM，EC50 为 16 μM) 具有高度选择性。Rivanicline hydrochloride 能够显著恢复学习障碍和认知功能障碍。Rivanicline hydrochloride 可用于研究神经退行性疾病 (如精神分裂症或阿尔茨海默病)。

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Rivanicline hydrochloride Chemical Structure

Rivanicline hydrochloride Chemical Structure

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Rivanicline hydrochloride 的其他形式现货产品:

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Other Forms of Rivanicline hydrochloride:

Rivanicline hydrochloride 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rivanicline (RJR-2403) hydrochloride is a neuronal nicotinic receptor agonist. Rivanicline hydrochloride is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hydrochloride can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hydrochloride can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease)[1][2][3][4][5].

IC50 & Target[3]

α4β2

16 μM (EC50)

α4β4

50 μM (EC50)

α3β2

150 μM (EC50)

α7

240 μM (EC50)

α3β2α5

360 μM (EC50)

α3β4

NA μM (EC50)

体内研究
(In Vivo)

Rivanicline hydrochloride (75-125 µmol/kg, s.c., 单次给药) 能在小鼠生理测试组合模型中引起体温、呼吸频率、Y迷宫活动和听觉惊吓反应的下降，但效力显著低于尼古丁[2]。
Rivanicline hydrochloride (0-1.2 µmol/kg, s.c., 单次给药) 显著改善了东莨菪碱 (HY-N0296) 所致遗忘后的被动回避记忆保持，并增强了前脑胆碱能投射系统受损大鼠在八臂放射状迷宫模型中的工作记忆和参考记忆[2]。
Rivanicline hydrochloride (2 mg/kg, i.p., 单次给药) 在眨眼条件反射功能受损的模型中，恢复了小鼠的学习能力[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Scopolamine (1.3 μmol/kg) -induced passive amnesia model established in male wistar rats (200-220 g)[2]
Dosage: 0.06, 0.6, 6 µmol/kg
Administration: Subcutaneous Injections (s.c.), 30 min before testing
Result: Reversed scopolamine-induced amnesia, increasing step-through latency at 0.6 µmol/kg.
No effect at 0.06 or 6 µmol/kg.
Animal Model: Ibotenic acid lesion radial arm maze model established in male Sprague-Dawley rats (250–270 g) [2]
Dosage: 0, 0.3, 0.6, 0.9, 1.2 µmol/kg
Administration: Subcutaneous Injections (s.c.), 20 min before testing
Result: Improved working memory (place task) in lesioned rats.
Animal Model: Physiological test battery model established in C57BL/6 mice[2]
Dosage: 75, 100 and 125 µmol/kg
Administration: Subcutaneous Injections (s.c.), single dose
Result: Was 15-50x less potent than nicotine in reducing body temperature, respiration, and locomotor activity.
Animal Model: MK-801 (0.02 mg/kg)-induced impairment of eyeblink conditioning model established in C57Bl/6 mice (3-5 months)[4]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Rescues learning by activating presynaptic nAChRs to enhance glutamate release.
分子量

198.69

Formula

C10H15ClN2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Rivanicline hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RivaniclineRJR-2403MetanicotineRJR2403RJR 2403nAChRNicotinic acetylcholine receptorsHippocampusEyeblinkClassical conditioningNMDA receptorsNicotinic receptorsPaired-pulse facilitationMiceInhibitorinhibitorinhibit

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